AZD5153-6-Hydroxy-2-naphthoic-acid-AZD-5153-HNT-salt-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAZD5153 6-Hydroxy-2-naphthoic acidCat. No.: HY-100653ACAS No.: 1869912-40-2Synonyms: AZD-5153 HNT salt分式: CHNO分量: 667.75作靶点: Epigenetic Reader Domain作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C

2、1 month溶解性数据体外实验 DMSO : 34 mg/mL (50.92 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.4976 mL 7.4878 mL 14.9757 mL5 mM 0.2995 mL 1.4976 mL 2.9951 mL10 mM 0.1498 mL 0.7488 mL 1.4976 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶

3、解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.74 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.74 mM); Clear solut

4、ion1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.74 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 AZD5153 6-Hydroxy-2-naphthoic acidAZD5153的6-羟 -2-萘甲酸盐形式。AZD5153 种有效选择性，有服活性的BET/BRD4溴结构域抑制剂; 扰BRD4的IC50值为1.7nM。IC50 & Target IC50: 1.7 nM (BRD4

5、) 1体外研究 AZD5153 demonstrates a remarkable enhancement in potency for the displacement of full-length BRD4relative to BD1, with IC50 values of 5.0 nM and 1.6 M, respectively. AZD5153 potently disrupts BRD4 foci inU2OS cells with an IC50 value of 1.7 nM. AZD5153 efficiently down-regulates MYC protein

6、levels across thecell line panel irrespective of their sensitivity to AZD5153 1.体内研究 Administration of AZD5153 leads to tumor stasis or regression in multiple xenograft models of acute myeloidleukemia, multiple myeloma, and diffuse large B-cell lymphoma. AZD5153 treatment markedly impactstranscripti

7、onal programs of MYC, E2F, and mTOR 1.PROTOCOLAnimal Mice: Mice are treated with either vehicle (0.5% hydroxymethylcellulose, 0.1% Tween80) or AZD5153 by oralAdministration 1 gavage mini-pump infusion. For continuous administration of AZD5153, compound is solubilized in 20% v/vDMSO/60% v/v HP-B-CD i

8、n water, loaded into a mini pump and implanted subcutaneously in mice. Tumorfragments collected are snap frozen or fixed in 10% buffered formalin. Blood samples are collected from thesame mice and stabilized in EDTA. Plasma concentrations are determined by liquid chromatography/tandemmass spectromet

9、ry method 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Rhyasen GW, et al. AZD5153: A Novel Bivalent BET Bromodomain Inhibitor Highly Active against Hematologic Malignancies. MolCancer Ther. 2016 Nov;15(11):2563-2574.McePdfHeightCaution: Product has not been fully validated for medica